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Nucleoside analogues are prevalent in drug design and call for more diversified structures. Bicyclo[1.1.1]pentane (BCP) structure has recently found wide applications in drug discovery. However, incorporation of BCP fragment into nucleoside analogues is hitherto unknown. Thus, from readily available BCP-containing building blocks, six new compounds, including pyrimidine nucleoside analogues, purine nucleoside analogues, and  C -nucleoside analogues were prepared in 1–4 steps, generally with good yields.

Preparation of bicyclo[1.1.1]pentane-derived nucleoside analogues